ArticleBritish journal of pharmacology2004
Overexpression of beta 1-adrenoceptors in adult rat ventricular myocytes enhances CGP 12177A cardiostimulation: implications for 'putative' beta 4-adrenoceptor pharmacology.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
15 citing papers in PubMed.
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- Microtubule-Mediated Regulation of βCirculation research · 2023Article
- Elevated blood pressure, antihypertensive medications and bone health in the population: revisiting old hypotheses and exploring future research directions.Osteoporosis international : a journal established as result of cooperation between the European Foundation for Osteoporosis and the National Osteoporosis Foundation of the USA · 2022Article
- Genetic susceptibility, elevated blood pressure, and risk of atrial fibrillation: a Mendelian randomization study.Genome medicine · 2021Article
- Cardiomyocyte-myofibroblast contact dynamism is modulated by connexin-43.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2019Article
- Effect of apelin on the cardiac hemodynamics in hypertensive rats with heart failure.International journal of molecular medicine · 2014Article
- β-adrenergic receptor responsiveness in aging heart and clinical implications.Frontiers in physiology · 2014Review
- The complex regulation of tanshinone IIA in rats with hypertension-induced left ventricular hypertrophy.PloS one · 2014Article
- Mechanism of loss of Kv11.1 K+ current in mutant T421M-Kv11.1-expressing rat ventricular myocytes: interaction of trafficking and gating.Circulation · 2012Article
- Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling.Trends in pharmacological sciences · 2011Review
- A full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors.PloS one · 2010Article
- A study of antagonist affinities for the human histamine H2 receptor.British journal of pharmacology · 2008Article
- Epinephrine enhances the sensitivity of rat vagal chemosensitive neurons: role of beta3-adrenoceptor.Journal of applied physiology (Bethesda, Md. : 1985) · 2007Article
- Phosphodiesterase PDE3 blunts the positive inotropic and cyclic AMP enhancing effects of CGP12177 but not of noradrenaline in rat ventricle.British journal of pharmacology · 2006Article
- Positive inotropic and lusitropic effects mediated via the low-affinity state of beta1-adrenoceptors in pithed rats.British journal of pharmacology · 2005Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. CGP 12177A mediates cardiostimulation by activation of the 'putative' beta(4)-adrenoceptor; however, it has recently been reported that disruption of the beta(1)-adrenoceptor gene abolishes this effect. We have adenovirally overexpressed beta(1)-adrenoceptors in isolated, cultured adult rat ventricular cardiomyocytes and observed the inotropic potency of isoprenaline and CGP 12177A (in the presence of 1 microm propranolol). 2. Isoprenaline was a full inotropic agonist at rat ventricular myocytes (pD(2) 7.69+/-0.12). CGP 12177A was a nonconventional partial agonist (pD(2) 6.34+/-0.09), increasing inotropy and lusitropy, with an intrinsic activity of 0.34 and antagonised by bupranolol. 3. beta(1)-adrenoceptor overexpression enhanced the inotropic potency of isoprenaline by 11.7-fold (pD(2) 8.76+/-0.14) and CGP 12177A by 5.9-fold (7.11+/-0.10), respectively. Green fluorescent protein (GFP) overexpression did not alter the potency of isoprenaline or CGP 12177A (pD(2) 7.41+/-0.24 and pD(2) 6.60+/-0.50, respectively). 4. The cardiostimulant effects of CGP 12177A were enhanced by IBMX (phosphodiesterase inhibitor) and decreased by Rp-cAMPS (cAMP antagonist). CGP 12177A also increased cAMP levels. CGP 12177A but not isoprenaline initiated arrhythmias at lower concentrations following beta(1)-adrenoceptor overexpression. 5. (125)I-Cyanopindolol saturation binding in Adv.beta(1) myocytes demonstrated approximately 18-fold increase in beta(1)-adrenoceptors. (3)H-CGP 12177A saturation binding, in the presence of propranolol, increased approximately 5-fold following overexpression of beta(1)-adrenoceptors. 6. This study demonstrates enhanced cardiostimulation by CGP 12177A (in the presence of propranolol) in rat ventricular myocytes overexpressing beta(1)-adrenoceptors, mediated by a Gs/cAMP signalling pathway. 'Putative' beta(4)-adrenoceptor pharmacology appears to be mediated by activation of a novel affinity state of the beta(1)-adrenoceptor.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.